Spiro Benzodiazepine Substituted Fluorocoumarins as Potent Anti-Anxiety Agents

1,5-Benzodiazepines are one of the important class of tranquilizers. The fusion of heterocyclic systems like coumarins and indolines with the benzodiazepine seems quite encouraging for the synthesis of derivatives with enhanced anti-anxiety property. The benzodiazepine derivatives containing fluorin...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Russian journal of bioorganic chemistry 2021-03, Vol.47 (2), p.390-398
Hauptverfasser: Patagar, Dayanand, Uttarkar, Akshay, Patra, Swarna M., Patil, Jagadish H., Kusanur, Raviraj, Niranjan, Vidya, Kumar, H. G. Ashok
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:1,5-Benzodiazepines are one of the important class of tranquilizers. The fusion of heterocyclic systems like coumarins and indolines with the benzodiazepine seems quite encouraging for the synthesis of derivatives with enhanced anti-anxiety property. The benzodiazepine derivatives containing fluorine were synthesized and studied for their anti-anxiety activity on mice using plus maze apparatus with sodium pentabarbitone as the standard. Compound with mono substituted fluorine showed comparable anti-anxiety activity with the standard. The docking studies with Translocator protein (TSPO) (PDB: 4UC2) were done and further supported by molecular dynamics simulations. The in vivo test results are in well agreement with docking and molecular dynamics simulation studies.
ISSN:1068-1620
1608-330X
DOI:10.1134/S1068162021020199